Glucocorticoids - Adrenocortical Steroids Flashcards
15.10
Class - Prednisone
Glucocorticoid; Immunosuppressive agent
MOA of Prednisone (3)
Prodrug that must be activated in the liver to prednisolone
4X stronger anti-inflammatory than cortisol and causes less Na+ retention in the kidneys
Intermediate duration of action
SE of Prednisone (4)
Glucose intolerance, immunosuppression, osteoporosis, psychosis
Class - Fludrocortisone
Glucocorticoid (used for mineralocorticoid purposes)
MOA of Fludrocortisone (2)
10X stronger anti-inflammatory than cortisol but causes 125X more Na+ retention in the kidneys
Short duration of action
When do you use Fludrocortisone?
Used in patients w/ hypoaldosteronism
SE of Fludrocortisone (9)
Adrenal suppression, fluid/electrolyte abnormalities, metabolic changes, edema, HTN, osteoporosis, growth suppression in children, cataracts, behavioral changes
Metabolic sides effects of Glucocorticoids (3)
Truncal obesity; muscle wasting (aka “Central sparing, peripheral wasting”); Cushing syndrome; osteoporosis
Anti-inflammatory/immunosuppressive effects of Glucocorticoids (4)
- Decreased arachidonic acid metabolism, both PGs and LTs (decreased COX-2 mRNA and protein, decreased PLA2 activity)
- Decreased cytokine expression
- Decreased cell-adhesion molecule expression
- Decreased fibroblast DNA synthesis/proliferation
Tissues that respond to glucocorticoids (7)
Adrenals Liver Kidney Brain/CNS Vasculature Muscle Adipose tissue
Tx of glucocorticoids (9)
Replacement therapy Congenital adrenal hyperplasia (CAH) Inflammatory states Asthma Immunosuppressive (transplant) Skin diseases Ulcerative colitis Cancer chemotherapy Thrombocytopenia
What drug is used to compare anti-inflammatory potency (GR) and Na+ retaining potency (MR)?
Cortisol; binds to MR and GR
What is the duration of action for cortisol?
short
Potency of Triamcinolone
5x Anti-inflammatory potency (GR)
0 Na+ retaining potency (MR)
Intermediate duration of action
Potency of Betamethasone
25x Anti-inflammatory potency (GR)
0 Na+ retaining potency (MR)
Long duration of action